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Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.

Abstract:

A novel series of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidine-based cyclooxygenase-2 (COX-2) inhibitors, which have a different arrangement of substituents compared to the more common 1,2-diarylheterocycle based molecules, have been discovered. For example, 2-(butyloxy)-4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)pyrimidine (47), a member of the 2-pyrimidinyl ether series, has been shown to be a potent and selective inhibitor with a favourable pharmacokinetic profile, h...

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Publication status:
Published

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Publisher copy:
10.1016/j.bmcl.2009.02.085

Authors


Swarbrick, ME More by this author
Beswick, PJ More by this author
Gleave, RJ More by this author
Bingham, S More by this author
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Journal:
Bioorganic and medicinal chemistry letters
Volume:
19
Issue:
15
Pages:
4504-4508
Publication date:
2009-08-05
DOI:
EISSN:
1464-3405
ISSN:
0960-894X
URN:
uuid:4e5f4dcc-6a58-4eba-bf2d-7c316b705b50
Source identifiers:
34753
Local pid:
pubs:34753

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